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首页> 外文期刊>Ukrainian Biochemical Journal >Effect of 3-substituted 1,4-benzodiazepin-2-ones on bradykinin-induced smooth muscle contraction
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Effect of 3-substituted 1,4-benzodiazepin-2-ones on bradykinin-induced smooth muscle contraction

机译：3-取代的1,4-苯并二氮杂-2-酮对缓激肽诱导的平滑肌收缩的影响

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摘要

Biochemical properties of 3-substituted 1,4-benzodiazepine determined by the characteristics of their chemical structure. Influence of 3-substituted 1,4-benzodiazepin-2-ones on maximal normalized rate and amplitudes of isometric smooth muscle contraction in rats was investigated. Compounds MX-1775 and MX-1828 demonstrated the similar inhibition effect on bradykinin-induced contraction of smooth muscle like competitive inhibitor des-argsup9/sup-bradykinin-acetate to bradykinin Bsub2/sub-receptors. MX-1626 demonstrated unidirectional changes of maximal normalized rate and force of smooth muscle that proportionally depended on bradykinin concentration in the range 10sup-10/sup-10sup-6/sup M. MX-1828 has statistically significant decrease of normalized rate of smooth muscle contraction for bradykinin concentrations 10sup-10/sup and 10sup-9/sup M by 20.7 and 8.6%, respectively, but for agonist concentration 10sup-6/sup M, this parameter increased?by 10.7% and amplitude was reduced?by 29.5%. Compounds MX-2011, MX-1785 and MX-2004 showed no natural effect on bradykinin-induced smooth muscle contraction. Compounds MX-1775, MX-1828, MX-1626 were selected for further research of their influence on kinin-kallikrein system and pain perception.
机译：3-取代的1，4-苯并二氮杂卓的生化特性由其化学结构特征决定。研究了3-取代的1,4-苯并二氮杂-2-酮对大鼠最大归一化率和等距平滑肌收缩幅度的影响。化合物MX-1775和MX-1828对缓激肽诱导的平滑肌收缩具有类似的抑制作用，如竞争性抑制剂des-arg 9 -缓激肽乙酸盐对缓激肽B 2 的抑制作用-受体。 MX-1626表现出最大归一化速率和平滑肌力量的单向变化，该变化与缓激肽浓度在10 -10 -10 -6 M范围内成比例。MX-1828缓激肽浓度10 -10 和10 -9 M分别使平滑肌收缩的标准化速率下降20.7％和8.6％，而激动剂浓度10 -6 M，此参数增加了10.7％，振幅降低了29.5％。化合物MX-2011，MX-1785和MX-2004对缓激肽诱导的平滑肌收缩没有天然作用。选择了化合物MX-1775，MX-1828，MX-1626，以进一步研究其对激肽激肽释放酶系统和疼痛感觉的影响。

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